External components

Abstract

To provide an external composition that has no stickiness and is good in use feeling and appearance (transparency) by allowing the coexistence of a heparin analog with one or more selected from 1,3-propanediol, a C5-10 alkanediol and an amphiphilic component.SOLUTION: An external composition is prepared that contains (A) a heparin analog and B) one or more selected from 1,3-propanediol, a C5-10 alkanediol and an amphiphilic component.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an external composition. More specifically, the present invention relates to an external composition containing a heparin analogue.

Background Art

[0002] Heparin analogues are one of the acidic mucopolysaccharides and have excellent moisturizing, anti-inflammatory, and blood circulation promoting effects, so they are widely used as active ingredients in external preparations.

[0003] For example, Patent Document 1 proposes a skin external composition characterized by containing a heparin analogue, a carboxyvinyl polymer and / or its salt, and xanthan gum. <000>

[0004] Further, Patent Document 2 proposes an external composition containing (A) a phosphocholine group-containing polymer, (B) hydroxypropylmethylcellulose, and (C) a heparin analogue.

Prior Art Documents

Patent Documents

[0005]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0006] Thus, in order to effectively exert the diverse efficacy of heparinoids, various formulations containing heparinoids have been developed. While these formulations were sufficient to impart the various pharmacological effects of heparinoids (such as the treatment and prevention of atopic dermatitis, hypertrophic scars and keloids, and post-traumatic care (bruises, sprains, contusions), concerns about the stickiness and irritation characteristic of mucopolysaccharides made it challenging to achieve a good user experience, especially in lotions. Furthermore, in liquid compositions such as lotions, various user experiences such as refreshing or moisturizing are desired depending on the purpose, but stickiness and irritation are generally undesirable in any case. In addition, in liquid compositions, the appearance of the formulation is also an important factor along with the user experience, and formulations with a transparent to translucent appearance were particularly desired to give a fresh appearance.

[0007] Therefore, given the above circumstances, the challenge was to obtain a transparent topical composition that possesses the diverse efficacy of heparin-like substances while also having a good feel (non-sticky) and appearance (transparency). Furthermore, the present invention aims to provide a transparent topical composition that also exhibits excellent stability. [Means for solving the problem]

[0008] The inventors of this invention have conducted extensive research to solve the above problems, We have discovered that by combining (A) a heparin-like substance and (B) one or more substances selected from 1,3-propanediol, alkanediols with 5 to 10 carbon atoms, and amphiphilic components, an external composition can be obtained that is non-sticky, has a good feel, and a good appearance (transparency). Furthermore, we have found that high stability (pH, color, transparency) can be ensured even under harsh conditions such as high temperature and light irradiation, thus completing the present invention.

[0009] In other words, the present invention provides the following external compositions. Section 1. (A) Heparin-like substances; (B) One or more selected from 1,3-propanediol, alkanediol with 5 to 10 carbon atoms, and amphiphilic components. A topical composition containing [a specific ingredient]. Section 2. The topical composition according to item 1, wherein the content of component (A) is 0.01 to 5% by mass. Section 3. The topical composition according to claim 1 or 2, wherein component (B) is one or more selected from the group consisting of 1,3-propanediol, alkanediol having 5 to 10 carbon atoms, (eicosanedioic acid / tetradecanedioic acid) decaglyceryl, bisethoxydiglycol cyclohexanedicarboxylic acid, diethylhexyl succinate, diethoxyethyl succinate, polyoxyalkylene glyceryl ether, polyoxyalkylene diglyceryl ether, polyoxyalkylene alkyl ether, and polyoxyalkylene alkyl glucoside. Item 4. The topical composition according to Item 3, wherein component (B) is one or more selected from the group consisting of 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, cyclohexanedicarboxylic acid bisethoxydiglycol, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene polyoxypropylene butyl ether, polyoxyethylene methyl glucoside, and polyoxypropylene methyl glucoside. Item 5. The topical composition according to any one of Items 1 to 4, further comprising component (C) one or more selected from the group consisting of glycyrrhizinate, water-soluble ascorbic acid derivatives, and tranexamic acid. Item 6. The topical composition according to Item 5, wherein the component (C) contains one or more selected from the group consisting of dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, sodium ascorbic acid phosphate, magnesium ascorbic acid phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid glucoside, and tranexamic acid. Item 7. The topical composition according to any one of Items 1 to 6, further containing component (D) liquid oil. Item 8. The topical composition according to any one of Items 1 to 7, characterized in that the topical composition is liquid. Item 9. The topical composition according to any one of Items 1 to 8, characterized in that the viscosity of the topical composition is 10 to 10000 mPa·s. Item 10. The topical composition according to any one of Items 1 to 10, characterized in that the appearance of the topical composition is transparent to translucent.

[0010] [Effects of the Invention]

[0011] The present invention provides an external composition that, by coexisting (A) a heparin-like substance and (B) one or more selected from 1,3-propanediol, alkanediols having 5 to 10 carbon atoms, and amphiphilic components, has a non-sticky feel and good appearance (transparency), and further ensures high stability (pH, color, transparency). [Modes for carrying out the invention]

[0012] Embodiments of the present invention will be described in detail below. However, the present invention is not limited to the following embodiments.

[0013] In this specification, the unit of content "mass%" is synonymous with "g / 100g".

[0014] The topical composition of the present invention contains (A) a heparin-like substance, and (B) one or more selected from 1,3-propanediol, an alkanediol having 5 to 10 carbon atoms, and an amphiphilic component.

[0015] [(A) Heparin-like substances] The heparin-like substance contained in the topical composition of the present invention refers to a general term for polysulfated mucopolysaccharides such as chondroitin polysulfate, and preferably has an average of 0.5 to 5 sulfate groups per monosaccharide molecule constituting the mucopolysaccharide, more preferably an average of 0.6 to 3 sulfate groups. More specifically, the heparin-like substance contains heparin, chondroitin sulfate D and chondroitin sulfate E, which are called chondroitin polysulfates.

[0016] Heparin-like substances can be obtained by sulfating mucopolysaccharides, or by extracting and purifying them from the internal organs, including the bronchi, of animals such as cattle and pigs using an aqueous carrier, followed by sulfation as needed. Since heparin-like substances have been developed as pharmaceutical or cosmetic ingredients, commercially available products can also be used.

[0017] In the topical composition of the present invention, as the heparin-like substance, those included in the Japanese Pharmaceutical Excipients Standards are preferably used.

[0018] In the topical composition of the present invention, the content of the component (A) relative to the total amount of the composition is appropriately set according to the types and contents of other compounding components, the dosage form, the method of use, etc. Preferably, it is 0.005% by mass or more, more preferably 0.001% by mass or more, still more preferably 0.01% by mass or more, and particularly preferably 0.1% by mass or more. The content of the heparin-like substance is preferably 10% by mass or less, more preferably 5% by mass or less, still more preferably 1% by mass or less, and particularly preferably 0.5% by mass or less with respect to the total amount of the composition. The content of the heparin-like substance is preferably 0.005 to 10% by mass, more preferably 0.001 to 5% by mass, still more preferably 0.01 to 1% by mass, and particularly preferably 0.1 to 0.5% by mass with respect to the total amount of the composition.

[0019] [(B) 1,3-propanediol, alkanediols having 5 to 10 carbon atoms, and amphiphilic components] As the component (B) of the present invention, 1,3-propanediol, alkanediols having 5 to 10 carbon atoms, and amphiphilic components are included in the liquid topical composition. By blending the component (B) together with the component (A), it becomes possible to provide a liquid topical composition in which good usability and formulation stability are compatible even when a heparin-like substance is blended. For example, 1,3-propanediol, alkanediols having 5 to 10 carbon atoms, (eicosanedioic acid / tetradecanedioic acid) decaglyceryl, bis(ethoxydiglycol) cyclohexanedicarboxylate, diethylhexyl succinate, diethoxyethyl succinate, polyoxyalkylene glyceryl ether, polyoxyalkylene diglyceryl ether, polyoxyalkylene alkyl ether, and polyoxyalkylene alkyl glucoside, etc. may be mentioned.

[0020] As component (B) of the present invention, any one of these compounds or a combination of two or more may be used, but preferably one or more selected from the group consisting of 1,3-propanediol, C5-C8 alkanediool, cyclohexanedicarboxylic acid bisethoxydiglycol, polyoxyalkylene glyceryl ether, polyoxyalkylene alkyl ether, and polyoxyalkylene alkyl glucoside. 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediool, cyclohexanedicarboxylic acid bisethoxydiglycol, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene alkyl ether, and one or more selected from the group consisting of polyoxyethylene methyl glucoside and polyoxypropylene methyl glucoside, and more preferably 1,3-propanediol One or more selected from the group consisting of 1,2-pentanediol, 1,2-hexanediol, cyclohexanedicarboxylic acid bisethoxydiglycol, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene polyoxypropylene butyl ether, polyoxyethylene methyl glucoside, and polyoxypropylene methyl glucoside is more preferable.

[0021] From the viewpoint of significantly exhibiting the effects of the present invention, the alkanediol having 5 to 10 carbon atoms preferably has 5 to 8 carbon atoms, more preferably 5 to 6. For example, one or more selected from the group consisting of 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediool are preferred, one or more selected from the group consisting of 1,2-pentanediol and 1,2-hexanediol are more preferred, and 1,2-pentanediol is even more preferred. In addition, commercially available products are not particularly limited, but HYDROLITE-5, HYDROLITE-5 Green (manufactured by Simrise Co., Ltd.), KMO-6 (manufactured by Osaka Organic Chemical Industry Co., Ltd.), Microcare Emollient PTGJ, Microcare Emollient HXD (manufactured by THOR), etc. can be used.

[0022] Amphiphilic compounds refer to all compounds that possess both hydrophilic and hydrophobic (lipophilic) groups within a single molecule, resulting in affinity for both the aqueous and oil (organic) phases.

[0023] Such amphiphilic components are not particularly limited, but examples include divalent carboxylic acid esters and alkylene oxide derivatives.

[0024] Divalent carboxylic acid esters are compounds formed by condensation of a divalent carboxylic acid with a hydroxyl group such as glyco or glyco ether, and are not particularly limited, but examples include (eicosanedioic acid / tetradecanediic acid) polyglyceryl-10, cyclohexanedicarboxylic acid bisethoxydiglycol, 1,4-cyclohexanedicarboxylic acid bis(triethyleneglycol monoethyl ether), adipic acid bis(diethyleneglycol monoethyl ether), adipic acid bis(triethyleneglycol monoethyl ether), and diethoxyethyl succinate and diethylhexyl succinate. Among these, one or more selected from the group consisting of (eicosanedioic acid / tetradecanedioic acid) polyglyceryl-10, cyclohexanedicarboxylic acid bisethoxydiglycol, diethoxyethyl succinate, and diethylhexyl succinate are preferred, one or more selected from the group consisting of diethoxyethyl succinate, eicosanedioic acid / tetradecanedioic acid) polyglyceryl-10, and cyclohexanedicarboxylic acid bisethoxydiglycol are more preferred, and diethoxyethyl succinate and cyclohexanedicarboxylic acid bisethoxydiglycol are even more preferred. In addition, commercially available products that are not particularly limited include diethoxyethyl succinate (CRODAMOL DES), diethylhexyl succinate (CRODAMOL OSU) (both manufactured by Croda Japan Co., Ltd.), Neosolue-Aqua·Neosolue-AquaS ((eicosanedioic acid / tetradecanedioic acid) polyglyceryl-10), and Neosolue-Aqulio (cyclohexanedicarboxylic acid bisethoxydiglycol) (both manufactured by Nippon Seika Co., Ltd.).

[0025] The alkylene oxide derivatives used in the present invention are polymers of specific alkylene glycols, or compounds obtained by adding a specific alkylene oxide group to a specific hydroxyl compound.

[0026] Among the alkylene oxide derivatives used in the present invention, those that significantly exhibit the effects of the present invention include polyoxyalkylene glyceryl ether, polyoxyalkylene alkyl glucoside, polyoxypropylene alkyl ether, polyoxyalkylene sorbitol, polyoxyalkylene erythritol ether, polyoxyalkylene pentaerythritol ether, polyoxyalkylene diglyceryl ether, polyoxyalkylene trimethylolpropane, polyoxypropylene glycol, polyoxyethylene polyoxypropylene glycol, polyoxyalkylene xylitol, polyoxyalkylene dipentaerythritol, polyoxyalkylene inositol, polyoxyalkylene sucrose ether, polyoxyalkylene trehalose ether, and polyoxyalkylene maltoitol ether.

[0027] Among them, alkylene oxide derivatives include polyoxyethylene glyceryl ether, polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene alkyl glucoside, polyoxyethylene polyoxypropylene alkyl glucoside, polyoxyethylene alkyl glucoside, polyoxypropylene alkyl glucoside, polyoxypropylene alkyl ether, Polyoxyethylene polyoxypropylene alkyl ether, polyoxypropylene sorbitol, polyoxyethylene sorbitol, polyoxyethylene polyoxypropylene sorbitol, polyoxypropylene erythritol ether, polyoxyethylene pentaerythritol ether, polyoxyethylene polyoxypropylene erythritol ether, polyoxypropylene pentaerythritol ether, polyoxyethylene polyoxypropylene pentaerythritol ether, polyoxybutylene Polyoxyethylene pentaerythritol ether, polyoxyethylene diglyceryl ether, polyoxypropylene diglyceryl ether, polyoxyethylene polyoxypropylene diglyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene diglyceryl ether, polyoxyethylene trimethylolpropane, polyoxypropylene trimethylolpropane, polyoxyethylene polyoxypropylene trimethylolpropane, polyoxypropylene glyco, polyoxyethylene polyoxypropylene glyco Polyoxybutylene polyoxyethylene polyoxypropylene glycol, polyoxyethylene xylitol, polyoxypropylene alkylene xylitol, polyoxyethylene polyoxypropylene xylitol, polyoxyethylene polyoxypropylene dipentaerythritol, polyoxyethylene dipentaerythritol, polyoxyethylene dipentaerythritol, polyoxyethylene inositol, polyoxypropylene inositol, polyoxyethylene polyoxypropylene inositol, polyoxyethylene sucrose ether,Preferably, one or more selected from the group consisting of polyoxypropylene scroether, polyoxyethylene polyoxypropylene scroether, polyoxyethylene trehalose ether, polyoxypropylene trehalose ether, polyoxyethylene polyoxypropylene trehalose ether, polyoxyethylene multi-thor ether, polyoxypropylene multi-thor ether, and polyoxyethylene polyoxypropylene multi-thor ether, Polyoxyethylene glyceryl ether, polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene alkyl glucoside, polyoxyethylene alkyl glucoside, polyoxypropylene alkyl glucoside, polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxypropylene sorbitol, polyoxyethylene sorbitol, polyoxyethylene polyoxypropylene pentaerythritol ether, polyoxypropylene pentaerythritol One or more selected from the group consisting of litol ether, polyoxyethylene pentaerythritol ether, polyoxybutylene polyoxyethylene pentaerythritol ether, polyoxyethylene diglyceryl ether, polyoxypropylene diglyceryl ether, polyoxyethylene polyoxypropylene diglyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene diglyceryl ether, polyoxyethylene polyoxypropylene trimethylolpropane, polyoxypropylene glycol, polyoxyethylene polyoxypropylene glycol, and polyoxybutylene polyoxyethylene polyoxypropylene glycol is more preferable. Polyoxyethylene glyceryl ether, polyoxypropylene glyceryl ether, polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene alkyl glucoside, polyoxypropylene alkyl glucoside, polyoxyethylene alkyl glucoside, polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxypropylene sorbitan More preferably, one or more selected from the group consisting of polyoxyethylene polyoxypropylene sorbitol, polyoxyethylene diglyceryl ether, polyoxypropylene diglyceryl ether, polyoxyethylene polyoxypropylene diglyceryl ether, polyoxybutylene polyoxyethylene polyoxypropylene diglyceryl ether, polyoxypropylene glycol, polyoxyethylene polyoxypropylene glycol, and polyoxybutylene polyoxyethylene polyoxypropylene glycol, One or more selected from the group consisting of polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether, polyoxypropylene alkyl glucoside, polyoxyethylene alkyl glucoside, and polyoxyethylene polyoxypropylene alkyl ether is more preferable.

[0028] The molecular weight of such alkylene oxide derivatives is not limited as long as the effects of the present invention are achieved, but from the viewpoint of significantly achieving the effects of the present invention, it is preferably 200 or more, more preferably 300 or more, and even more preferably 400 or more.

[0029] The properties of the alkylene oxide derivative are not limited as long as they achieve the effects of the present invention, but from the viewpoint of significantly achieving the effects of the present invention, it is preferable that the component is semi-solid (including paste-like) to liquid at 25°C.

[0030] Among the alkylene oxide derivatives, the polyoxyalkylene alkyl ether is preferably polyoxyethylene, and preferably a component that is semi-solid (including paste-like) to liquid at 25°C.

[0031] Among these alkylene oxide derivatives, polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether is preferably polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether (3B.O.) (8E.O.) (5P.O.).

[0032] Among these alkylene oxide derivatives, the polyoxyalkylene alkyl glucoside is preferably one or more selected from the group consisting of polyoxyethylene methyl glucoside and polyoxypropylene methyl glucoside, and more preferably one or more selected from the group consisting of polyoxypropylene methyl glucoside (10P.O.), polyoxypropylene methyl glucoside (20P.O.), polyoxyethylene methyl glucoside (10P.O.), and polyoxyethylene methyl glucoside (20P.O.).

[0033] Among these alkylene oxide derivatives, the polyoxyethylene polyoxypropylene alkyl ether is preferably one or more selected from the group consisting of polyoxyethylene polyoxypropylene butyl ether, polyoxyethylene polyoxypropylene cetyl ether, and polyoxyethylene polyoxypropylene decyltetradecyl ether, such as polyoxyethylene polyoxypropylene butyl ether (17E.O.) (17P.O.) and polyoxyethylene polyoxypropylene butyl ether (37E.O.) ( One or more of the following are more preferably selected from the group consisting of 38P.O.), polyoxyethylene polyoxypropylene cetyl ether (10E.O.) (8P.O.), polyoxyethylene polyoxypropylene decyltetradecyl ether (30E.O.) (6P.O.), polyoxyethylene polyoxypropylene decyltetradecyl ether (20E.O.) (6P.O.), polyoxyethylene polyoxypropylene decyltetradecyl ether (24E.O.) (13P.O.), and polyoxyethylene polyoxypropylene decyltetradecyl ether (10E.O.) (6P.O.).

[0034] These alkylene oxide derivatives include Unilube 50MB-26 (polyoxyethylene polyoxypropylene butyl ether (17 E.O.) (17 P.O.)), Unilube 50MB-168 (polyoxyethylene polyoxypropylene butyl ether (37 E.O.) (38 P.O.)), Unilube 50MB-11 (polyoxyethylene polyoxypropylene butyl ether (9 E.O.) (10 P.O.)), Unisafe 10P-8 (polyoxyethylene polyoxypropylene cetyl ether (10 E.O.) (8 P.O.)), Unilube MT-630B (polyoxyethylene polyoxypropylene decyltetradecyl ether (30 E.O.) (6 P.O.)), and Unilube 50MT-2200B (polyoxyethylene polyoxy Cypropylene decyltetradecyl ether (24 E.O.) (13 P.O.), Unilube 20MT-2000B (Polyoxyethylene polyoxypropylene decyltetradecyl ether (24 E.O.) (13 P.O.)), Unilube MS-70K (Polyoxypropylene stearyl ether (15 P.O.)), Uniol HS-1600D (Polyoxyalkylene sorbitol), Pronon #208 (Polyoxyethylene polyoxypropylene glycol (15 0E.O.)(35P.O.)), Pronon #124P (Polyoxyethylene (20) Polyoxypropylene (20) Glycol), Uniol D-2000 (Polypropylene Glycol), Macbiobride MG-10E (Polyoxyethylene Methyl Glucoside (10E.O.)), Macbiobride MG-20E (Polyoxyethylene Methyl Glucoside (20E.O.)), Macbiobride MG-10P (Polyoxypropylene Methyl Glucoside (10P.O.)) MacBioBride MG-20P (Polyoxypropylene Methyl Glucoside (20 P.O.)), Wilbride MG2070 (Polyoxybutylene Polyoxyethylene Polyoxypropylene Methyl Glucoside), Unilube 5TP-300KB (Polyoxyethylene Polyoxypropylene Pentaerythritol Ether (5 E.O.) (65 P.O.)); Unilube 50TG-32 (Polyoxyethylene Polyoxypropylene Glyceryl Ether (24 E.O.) (24 P.O.))), Wilbride S-753 (polyoxybutylene polyoxyethylene polyoxypropylene glyceryl ether (3B.O.) (8E.O.) (5P.O.)), Uniox G-1200 (polyoxyethylene glycerin), Unilube DGP-700, Unilube DGP-950 (polyoxypropylene diglyceryl ether) (all manufactured by NOF Corporation); SY-DP14, SY-DP9 (polyoxypropylene diglyceryl ether) (all manufactured by Sakamoto Pharmaceutical Co., Ltd.); Newport GP-1000 (PPG-16 glyceryl ether), Newport SP-750 (polyoxyalkylene sorbitol ether), Newport PE-68 (polyoxyethylene Polyoxypropylene glycol (160 E.O.) (30 P.O.), Newport PE-78 (polyoxyethylene polyoxypropylene glycol (150 E.O.) (35 P.O.)), Newport GEP-2800 (polyoxyethylene polyoxypropylene glyceryl ether (24 E.O.) (24 P.O.)) (all manufactured by Sanyo Chemical Industries, Ltd.); Emulgen PP-290 (polyoxyethylene polyoxypropylene glycol (160 E.O.) (30 P.O.), manufactured by Kao Corporation); NIKKOL These products are commercially available under names such as SG-G2424 (polyoxyethylene polyoxypropylene glyceryl ether (24 E.O.) (24 P.O.)), NIKKOL SG-DTD630 (polyoxyethylene polyoxypropylene decyltetradecyl ether (30 E.O.) (6 P.O.)) (manufactured by Nikko Chemicals); GLUCAM P-10 (polyoxypropylene methyl glucoside (10 P.O.)), GLUCAM P-20 (polyoxypropylene methyl glucoside (20 P.O.)), GLUCAM E-10 (polyoxyethylene methyl glucoside (10 P.O.)), and GLUCAM E-20 (polyoxyethylene methyl glucoside (20 P.O.)) (manufactured by Lubrizol).

[0035] In the present invention, one alkylene oxide derivative may be used alone, or two or more derivatives may be used in any combination.

[0036] In the topical composition of the present invention, the total content of component (B) is not particularly limited and is set appropriately depending on the types of other components, etc., but from the viewpoint of significantly achieving the effects of the present invention, it is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.5% by mass or more, and even more preferably 1% by mass or more, based on the total amount of the composition. The total content of component (B) is preferably 30% by mass or less, more preferably 20% by mass or less, even more preferably 15% by mass or less, even more preferably 10% by mass or less, and most preferably 5% by mass or less, based on the total amount of the composition. The total content of component (B) is preferably 0.01 to 30% by mass, more preferably 0.1 to 20% by mass, even more preferably 0.5 to 15% by mass, even more preferably 0.5 to 10% by mass, and most preferably 0.5 to 5% by mass, based on the total amount of the composition.

[0037] In the external composition of the present invention, the ratio of the total content of component (B) to component (A) is not particularly limited, but the amount of component (B) is preferably 0.01 to 50,000 parts by mass, more preferably 0.1 to 20,000 parts by mass, even more preferably 0.5 to 1,000 parts by mass, and even more preferably 1 to 300 parts by mass per 1 part by mass of component (A).

[0038] In the topical composition of the present invention, the amount of 1,3-propanediol alone relative to the total amount of the composition is not particularly limited as long as the effects of the present invention are achieved. The content of 1,3-propanediol alone is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, even more preferably 0.1% by mass or more, and even more preferably 0.5% by mass or more, based on the total amount of the composition. The content of 1,3-propanediol alone is preferably 20% by mass or less, more preferably 10% by mass or less, and even more preferably 5% by mass or less, based on the total amount of the composition. The content of 1,3-propanediol alone is preferably 0.001% to 20% by mass, more preferably 0.001 to 10% by mass, even more preferably 0.01 to 8% by mass, and even more preferably 0.1% to 5% by mass, based on the total amount of the composition.

[0039] In the topical composition of the present invention, the individual content of 1,3-propanediol and / or alkanediol having 5 to 10 carbon atoms relative to the total amount of the composition is not particularly limited as long as the effects of the present invention are achieved. The content of each alkanediol having 5 to 10 carbon atoms is preferably 0.001% by mass or more, more preferably 0.001% by mass or more, even more preferably 0.01% by mass or more, and even more preferably 0.1% by mass or more, relative to the total amount of the composition. The content of each alkanediol having 5 to 10 carbon atoms is preferably 10% by mass or less, more preferably 5% by mass or less, and even more preferably 3% by mass or less, based on the total amount of the composition. The individual content of alkanediols having 5 to 10 carbon atoms is preferably 0.001 to 10% by mass, more preferably 0.001 to 7% by mass, even more preferably 0.01 to 5% by mass, and even more preferably 0.1% to 3% by mass, relative to the total amount of the composition.

[0040] In the topical composition of the present invention, the content of cyclohexanedicarboxylic acid bisethoxydiglycol alone relative to the total amount of the composition is not particularly limited as long as the effects of the present invention are achieved. The content of cyclohexanedicarboxylic acid bisethoxydiglycol alone is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, even more preferably 0.01% by mass or more, and even more preferably 0.05% by mass or more, based on the total amount of the composition. The content of cyclohexanedicarboxylic acid bisethoxydiglycol alone is preferably 10% by mass or less, more preferably 8% by mass or less, and even more preferably 5% by mass or less, based on the total amount of the composition. The content of cyclohexanedicarboxylic acid bisethoxydiglycol alone is preferably 0.001 to 10% by mass, more preferably 0.005 to 8% by mass, even more preferably 0.01 to 5% by mass, and even more preferably 0.05% to 3% by mass, based on the total amount of the composition.

[0041] In the topical composition of the present invention, the content of the alkylene oxide derivative alone relative to the total amount of the composition is not particularly limited as long as the effects of the present invention are achieved. The content of the alkylene oxide derivative alone is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, and even more preferably 1% by mass or more, based on the total amount of the composition. The content of the alkylene oxide derivative alone is preferably 15% by mass or less, more preferably 10% by mass or less, and even more preferably 8% by mass or less, based on the total amount of the composition. The content of the alkylene oxide derivative alone is preferably 0.01 to 15% by mass, more preferably 0.1 to 10% by mass, and even more preferably 1 to 8% by mass, based on the total amount of the composition.

[0042] [(C) One or more selected from the group consisting of glycyrrhizinate, water-soluble ascorbic acid derivatives, tranexamic acid, and nicotinamide] Furthermore, as component (C) of the present invention, one or more selected from the group consisting of glycyrrhizinate, water-soluble ascorbic acid derivatives, and tranexamic acid can be included in a transparent to translucent topical composition. Component (C) is an ingredient that has diverse efficacy such as anti-inflammatory and whitening effects, but all of them are ingredients that may cause stickiness. In the present invention, even if component (C) is combined with component (A), a good feel can be maintained without stickiness.

[0043] Glycyrrhizinate is not particularly limited, but examples include dipotassium glycyrrhizinate and monoammonium glycyrrhizinate, with dipotassium glycyrrhizinate being preferred.

[0044] The water-soluble ascorbic acid derivatives are not particularly limited, but examples include sodium ascorbate phosphate, magnesium ascorbate phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid glucoside, disodium isostearyl ascorbyl phosphate, glyceryl ascorbic acid, bisglyceryl ascorbic acid, alkylglyceryl ascorbic acid, etc., among which one or more selected from the group consisting of sodium ascorbate phosphate, magnesium ascorbate phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, and ascorbic acid glucoside are preferred, and one or more selected from the group consisting of sodium ascorbate phosphate, magnesium ascorbate phosphate, 3-O-ethyl ascorbic acid, ascorbic acid glucoside, and 2-O-ethyl ascorbic acid are more preferred.

[0045] Such (C) components are not particularly limited, but examples include one or more selected from the group consisting of dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, sodium ascorbate phosphate, magnesium ascorbate phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbate glucoside, disodium isostearyl ascorbyl phosphate, glyceryl ascorbate, bisglyceryl ascorbate, alkylglyceryl ascorbate, tranexamic acid, and nicotinamide, among which dipotassium glycyrrhizinate and glycyrrhizinate are selected. Preferably, one or more selected from the group consisting of monoammonium ascorbate, sodium ascorbate phosphate, magnesium ascorbate phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbate glucoside, tranexamic acid, and nicotinamide is used, and more preferably, one or more selected from the group consisting of dipotassium glycyrrhizinate, sodium ascorbate phosphate, magnesium ascorbate phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbate glucoside, tranexamic acid, and nicotinamide is used.

[0046] In the transparent to translucent topical composition of the present invention, the total content of component (C) relative to the total amount of the composition is preferably 0.001 to 10% by mass, more preferably 0.005 to 5% by mass, even more preferably 0.01 to 3% by mass, and even more preferably 0.05 to 2% by mass.

[0047] In the transparent to translucent external composition of the present invention, the ratio of the total content of component (C) to component (A) is not particularly limited, but preferably 0.0001 to 5000 parts by mass, more preferably 0.01 to 100 parts by mass, and even more preferably 0.1 to 20 parts by mass of component (C) per 1 part by mass of component (A).

[0048] [(D) Liquid oil] Furthermore, as component (D) of the present invention, one or more liquid oils may be included in the topical composition of the present invention. Liquid oils are ingredients that give the formulation a plump and smooth feel, as well as a moderate moisturizing effect. In the present invention, component (D) may be included in the topical composition of the present invention to an extent that does not impair the transparency of the appearance.

[0049] Furthermore, the liquid oil component (D) of the present invention refers to an oil that is liquid at 25°C. Such component (D) is not particularly limited, but examples include ester oils, vegetable oils, animal oils, oil-soluble vitamins, hydrocarbon oils, higher fatty acids, higher alcohols, alkylglyceryl ethers, silicone oils, fluorinated oils, lanolin, and lanolin derivatives. Specifically, these include ester oils of linear fatty acids and lower alcohols such as diethyl sebacate, isopropyl myristate, butyl myristate, isopropyl palmitate, ethyl stearate, butyl stearate, ethyl oleate, ethyl linoleate, and isopropyl linoleate; ester oils of linear fatty acids and higher linear alcohols such as cetyl caprate, hexyl laurate, decyl myristate, myristyl myristate, cetyl myristate, cetyl palmitate, stearyl stearate, decyl oleate, and oleyl oleate; and octyl myristate. Ester oils of straight-chain fatty acids such as dodecyl, 2-ethylhexyl palmitate, isocetyl palmitate, isostearyl palmitate, 2-ethylhexyl stearate, isocetyl stearate, isodecyl oleate, octyldodecyl oleate, octyldodecyl ricinoleate, etc., with branched-chain alcohols; ester oils of branched-chain fatty acids such as ethyl isostearate, isopropyl isostearate, etc., with lower alcohols; ester oils of branched-chain fatty acids such as cetyl 2-ethylhexanoate, cetostearyl 2-ethylhexanoate, stearyl 2-ethylhexanoate, hexyl isostearate, 2-hexyldecyl isostearate, etc., with straight-chain higher alcohols;Ethylene glycoside dioctanoate, ethylene glycoside dioleate, propylene glycoside caprylate, propylene glycoside dicaprylate, di(caprylic / capric acid) propylene glycoside, propylene glycoside dicaprate, dipropylene glycoside dioleate, neopentyl glycoside dicaprate, neopentyl glycoside dioctanoate, glyceryl tricaprylate, glyceryl tri-2-ethylhexanoate, tri(caprylic / capric acid) glyceryl, tri Fatty acids and polyvalents such as glyceryl isopalmitate, glyceryl triisostearate, glyceryl tri(caprylate / caprate / myristic / stearate), glyceryl (ethylhexanoate / stearate / adipate), trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, pentaerythritol tetra-2-ethylhexanoate, pentaerythritol tetraisostearate, and pentaerythritol tetra-2-ethylhexanoate. Ester oils with alcohol; ester oils of branched fatty acids and branched alcohols such as octyldodecyl neopentanoate, isocetyl octanoate, isostearyl octanoate, 2-ethylhexyl isoperargonic acid, hexyldecyl dimethyloctanoate, octyldodecyl dimethyloctanoate, 2-ethylhexyl isopalmitate, isocetyl isostearate, isostearyl isostearate, octyldodecyl isostearate, lauryl lactate, myris lactate Hydroxyl ester oils such as cetyl lactate, octyldodecyl lactate, trioctyl citrate, triisocetyl citrate, trioctyldodecyl citrate, diisostearyl malate, trimethyl trimellitate; dibasic acid ester oils such as diethylhexyl succinate, diethoxyethyl succinate, dioctyl succinate, diisopropyl adipate, diisobutyl adipate, dioctyl adipate, diethyl sebacate, diisopropyl sebacate, dioctyl sebacate;Vegetable oils such as rapeseed oil, avocado oil, almond oil, olive oil, kukui nut oil, sesame oil, wheat germ oil, rice germ oil, rice bran oil, rice oil, safflower oil, sunflower oil, soybean oil, evening primrose oil, corn oil, rapeseed oil, persic oil, palm oil, palm kernel oil, castor oil, jojoba oil, grapeseed oil, macadamia nut oil, meadowfoam oil, barnyard grass oil, coconut oil, rosehip oil, etc.; liquid horse oil Animal oils such as mink oil and liquid lanolin; oil-soluble vitamins such as dl-α-tocopherol, dl-α-tocopherol succinate, dl-α-tocopherol nicotinate, dl-α-tocopherol acetate, benzyl nicotinate, ascorbyl tetra-2-hexyldecanoate, retinol acetate, retinol palmitate, retinol propionate; liquid paraffin, light liquid isoparaffin, heavy liquid isoparaffin Examples include linear or branched hydrocarbon oils such as paraffin, liquid isoparaffin, polybutene, polyisobutene, hydrogenated polyisobutene, squalane (including sugar-squalane), squalene, α-olefin oligomer, isohexadecane, and isododecane; higher fatty acids such as oleic acid and isostearic acid; higher alcohols such as isostearyl alcohol, octyldodecanol, and hexyldecanol; alkylglyceryl ethers such as isostearyl glyceryl ether; silicone oils such as methylpolysiloxane, dimethylpolysiloxane, dimethylcyclopolysiloxane, decamethylcyclopentasiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, and higher alcohol-modified silicone oil; and fluorinated oils such as fluoropolyether and perfluoroalkyl ether silicone.

[0050] Furthermore, as component (D) of the present invention, from the viewpoint of significantly exhibiting the effects of the present invention, hydrocarbon oils, ester oils, oil-soluble vitamins, and vegetable oils are preferred, including diethyl sebacate, isopropyl myristate, isopropyl palmitate, ethyl oleate, cetyl palmitate, decyl oleate, oleyl oleate, octyldodecyl myristate, 2-ethylhexyl palmitate, isopropyl palmitate, isostearyl palmitate, octyldodecyl oleate, isostearyl isostearate, cetyl 2-ethylhexanoate, and propyl caprylate. Polyglycerides, Propylene Glycol Dicaprylate, Di(Caprylic / Capric Acid) Propylene Glycol, Propylene Glycol Dicaprate, Dipropylene Glycol Dioleate, Neopentyl Glycol Dicaprate, Neopentyl Glycol Dioctanoate, Glyceryl Tricaprylate, Glyceryl Tri-2-Ethylhexanoate, Tri(Caprylic / Capric Acid) Glyceryl Tri(Caprylic / Capric Acid / Myristic Acid / Stearic Acid) Glyceryl Tri(Trimethylolpropane Tri-2-Ethylhexanoate, Trimethylolpane Triisostearate Ropan, Pentaerythritol Tetra-2-ethylhexanoate, Pentaerythritol Tetraisostearate, Pentaerythritol Tetra-2-ethylhexanoate, Octyldodecyl Neopentanoate, Triethyl Citrate, Triisocetyl Citrate, Trimethyl Trimellitate, Diisopropyl Adipate, Diethyl Sebacate, Diisopropyl Sebacate, Dioctyl Sebacate, Rapeseed Oil, Avocado Oil, Almond Oil, Olive Oil, Kukui Nut Oil, Sesame Oil, Wheat Germ Oil, Rice Germ Oil, Rice Bran Oil, Rice Oil, Safflower Oil, Sunflower Oil, Soybean Oil Evening primrose oil, corn oil, rapeseed oil, persic oil, palm oil, palm kernel oil, castor oil, jojoba oil, grapeseed oil, macadamia nut oil, meadowfoam oil, barnyard grass oil, coconut oil, rosehip oil, dl-α-tocopherol, dl-α-tocopherol succinate, dl-α-tocopherol nicotinate, dl-α-tocopherol acetate, benzyl nicotinate, ascorbyl tetra-2-hexyldecanoate, retinol acetate, retinol palmitate, retinol propionate, liquid paraffin, light liquid isoparaffin, heavy liquid isoparaffin,Liquid isoparaffin, squalane (including sugar-squalane), α-olefin oligomer, oleic acid, isostearic acid, isostearyl alcohol, octyldodecanol, hexyldecanol, isostearyl glyceryl ether are preferred, and more preferably one or more selected from liquid paraffin, liquid isoparaffin, α-olefin oligomer, propylene glycol caprylate, propylene glycol dicaprate, propylene glycol dicaprylate, dicapric acid Neopentyl Glycol, Glyceryl Tricaprylate, Glyceryl Tri-2-ethylhexanoate, Caprylic / Capric Triglyceride, Glyceryl Triisopalmitate, Glyceryl Triisostearate, Trimethylolpropane Tri-2-ethylhexanoate, Glyceryl Tri(Caprylic / Capric / Myristic / Stearic Acid), Trimethylolpropane Triisostearate, Pentaerythritol Tetra-2-ethylhexanoate, Pentaerythritol Tetraisostearate Toxol, pentaerythritol tetra-2-ethylhexanoate, avocado oil, olive oil, sesame oil, soybean oil, evening primrose oil, jojoba oil, grapeseed oil, macadamia nut oil, meadowfoam oil, dl-α-tocopherol, dl-α-tocopherol acetate, ascorbyl tetra-2-hexyldecanoate, retinol acetate, retinol palmitate, retinol propionate, isostearic acid, isostearyl alcohol, octyldodecanol, isostearyl glyceryl ether are even better. More preferably, liquid paraffin, liquid isoparaffin, α-olefin oligomer, glyceryl tri-2-ethylhexanoate, caprylic / capric triglyceride, trimethylolpropane tri-2-ethylhexanoate, glyceryl tri-caprylic / capric / myristic / stearic acid, evening primrose oil, jojoba oil, macadamia nut oil, meadowfoam oil, dl-α-tocopherol, dl-α-tocopherol acetate, and ascorbyl tetra-2-hexyldecanoate are used.

[0051] In the external composition of the present invention, the total content of component (D) relative to the total amount of the composition is preferably 0.0001 to 5% by mass, more preferably 0.0005 to 3% by mass, even more preferably 0.001 to 1% by mass, and even more preferably 0.01 to 0.5% by mass.

[0052] [Liquid Topical Composition] In this specification, "liquid topical composition" means a composition that is liquid or fluid at 25°C. For example, the formulation can be a liquid, suspension, emulsion, lotion, gel, liniment, lotion, aerosol, sheet impregnated with the drug solution, or mist. Among these, liquids, emulsions, gels, lotions, sheets, aerosols, and mists are preferred, and liquids, gels, lotions, sheets, aerosols, and mists are more preferred.

[0053] [Viscosity] The external composition of the present invention is preferably in the form of a liquid that is fluid at 25°C, and is preferably a lotion, but may also have properties in which viscosity is increased by adding a thickening agent. From this viewpoint, the viscosity (25°C) of the transparent external composition of the present invention is not particularly limited, but is preferably 10 to 10000 mPa·s, more preferably 10 to 5000 mPa·s, even more preferably 50 to 1000 mPa·s, and particularly preferably 500 mPa·s or less.

[0054] In this specification, viscosity (25°C) refers to the viscosity measured using a single-cylinder rotational viscometer (Brookfield type viscometer) in accordance with the viscosity measurement method described in the general test methods of the 17th edition of the Japanese Pharmacopoeia. Specifically, it refers to the value measured using the TV-10M (manufactured by Toki Sangyo Co., Ltd.), and the selection of conditions such as rotor and rotation speed shall be in accordance with the instruction manual of this instrument, and the viscosity at 25°C shall be measured.

[0055] The following is a description of a single-cylinder rotational viscometer. A single-cylinder rotational viscometer is a viscometer that measures the torque when a cylinder in a liquid is rotated at a constant angular velocity. The viscosity η of the liquid is calculated by the following formula, after experimentally determining the instrument constant KB using a viscometer calibration standard solution: η = KBX T / ω η: viscosity of the liquid (mPa·s) KB: instrument constant (rad / cm) 3 ) ω: angular velocity (rad / s) T: torque acting on the cylindrical surface (10 -7 N·m)

[0056] [Transparency] In this specification, "topical composition having a good appearance (transparency)" further means "a transparent to translucent topical composition" whose appearance is transparent or translucent when viewed visually. Furthermore, if the composition contains oil as a solubilizable component, the composition is such that the solubilizable component is in a solubilized state, and if the appearance is translucent, it also includes being in a microemulsion (fine emulsification) state. The appearance of the topical composition of the present invention is preferably transparent to translucent, and the solubilizable component in the composition is preferably in a solubilized state.

[0057] Here, "transparent to translucent" refers to a preference for a transparency indicator where the absorbance at 630 nm is less than 0.3. Absorbance can be measured using a microplate recorder (e.g., SH-9000, manufactured by Corona Electric Co., Ltd.). A lower absorbance indicates higher transmittance and thus higher transparency. In the "transparent to translucent external composition" of the present invention, when filled to a height of approximately 3 cm in a transparent glass bottle with a diameter of approximately 3 cm, the characters in font 14 (black text on a white background) written on the bottom of the bottle can be read. Among those with a translucent appearance, if they are in a microemulsion state, their appearance may be colorless to bluish-white, but even in that case, it can be determined whether they fall within the category of a "transparent to translucent external composition" by considering the absorbance and the visibility of the characters as described above. Preferably, the absorbance at 630 nm is 0.1 to 0.3 and the characters appear clear and sharp in the character recognition test; more preferably, the absorbance at 630 nm is 0.05 to 0.1 and the characters appear clear and sharp in the character recognition test; and even more preferably, the absorbance at 630 nm is less than 0.05.

[0058] [Other ingredients] In addition to the essential components mentioned above, the topical skin composition of the present invention may contain one or more of the following components in combination to add other beneficial effects: ultraviolet scattering agents, ultraviolet absorbing agents, components having DNA damage prevention and / or repair effects, whitening components, anti-inflammatory components, cooling agents, organic acids, anti-glycation components, antibacterial components, cell activating components, astringent components, antioxidant components, anti-aging components, moisturizing components, polyhydric alcohols, keratin softening components, vitamins, blood circulation promoting components, sebum-absorbing components, peptides or their derivatives, amino acids or their derivatives, etc. These components are not particularly limited as long as they can be used in the fields of pharmaceuticals, quasi-drugs, cosmetics, etc., and any of them can be appropriately selected and used. Furthermore, components falling under any of the following multiple components may be added as components with any of the following efficacy properties.

[0059] Examples of the aforementioned ultraviolet scattering agents include inorganic compounds such as zinc oxide, titanium oxide, iron oxide, cerium oxide, zirconium oxide, titanium silicate, zinc silicate, anhydrous silicic acid, cerium silicate, and hydrated silicic acid; inorganic compounds coated with hydrated silicic acid, aluminum hydroxide, mica, or talc; compounds compounded with resin powders such as polyamide, polyethylene, polyester, polystyrene, or nylon; and those treated with silicon oil or fatty acid aluminum salts.

[0060] The aforementioned ultraviolet absorbers are not limited to, but are preferably salicylic acid-based ultraviolet absorbers, cinnamic acid-based ultraviolet absorbers, benzoylmethane-based ultraviolet absorbers, benzoic acid ester derivative ultraviolet absorbers, triazine derivative ultraviolet absorbers, benzalmalonate derivative ultraviolet absorbers, octocrylene-based ultraviolet absorbers, imidazole sulfonic acid derivative ultraviolet absorbers, benzophenone derivative ultraviolet absorbers, and the like.

[0061] Furthermore, these UV scattering agents and UV absorbing agents may be compounded, supported, or encapsulated with other components, and the combinations thereof are not particularly limited.

[0062] Examples of components that have a preventive and / or repair effect on DNA damage include components derived from animals (e.g., Artemia); components derived from plants (e.g., cat's claw); and nucleic acid components such as DNA, DNA salts, RNA, and RNA salts.

[0063] Examples of whitening ingredients include nicotinamide, placenta, arbutin, kojic acid, ellagic acid, phytic acid, tranexamic acid, lucinol, chamomile ET, hydroquinone, potassium 4-methoxysalicylate, linoleic acid and its derivatives, vitamin C such as ascorbic acid and its salts, and ascorbic acid derivatives (sodium ascorbate phosphate, magnesium ascorbate phosphate, ascorbyl tetra-2-hexyldecanoate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid glucoside, disodium isostearyl ascorbyl phosphate, L-ascorbyl dipalmitate, trisodium ascorbyl palmitate phosphate, glyceryl ascorbate, bisglyceryl ascorbate, alkylglyceryl ascorbate, etc.), vitamin A or its derivatives, pantothenic acid or its derivatives, and other vitamins. Furthermore, plant-derived ingredients with whitening properties may be used as whitening ingredients. Such plant-derived ingredients include iris, almond, aloe, acerola, oolong tea, rosehip, scutellaria, coptis japonica, St. John's wort, deadnettle, seaweed, kudzu, gardenia, Sophora flavescens, chlorella, rice, rice husk, oryzanol, rice bran, Asarum sieboldii, Japanese pepper, perilla, peony, Cnidium officinale, mulberry bark, soybean, natto, tea, angelica, calendula, witch hazel, safflower, peony bark, coix seed, catechu, and persimmon (Diospyros). Examples of plant components include those derived from kaki, kiwi, black bean, gentian, genjin, sage, radish, azalea, parsley, holly, hops, thyme, clove, dried tangerine peel, licorice, chamomile, prune, meadowsweet, beautyberry, water chestnut, grapefruit, thornless, lemon, kiwi, pine, neem, artichoke, horsetail, Phellodendron bark, evening primrose, bilberry, geranium, glasswort, white willow, saxifrage, centella asiatica, rosemary, lavender, etc. When these plant components are used in the external composition of the present invention, the form of the plant components is not particularly limited, but they can usually be used in the form of plant extracts or essential oils. The names in parentheses in the above plant components are the scientific name, alternative name, or crude drug name of the plant.

[0064] When the whitening ingredients described above are incorporated into the topical composition of the present invention, their content can be appropriately selected considering the feel on the skin and the effect, but is, for example, about 0.0003 to 10% by mass, preferably about 0.01 to 5% by mass, relative to the total amount of the topical composition. When plant extracts are used, the content, in terms of extracts, is, for example, about 0.00001 to 20% by mass, preferably about 0.0001 to 15% by mass, more preferably 0.001 to 10% by mass, relative to the total amount of the topical composition.

[0065] Examples of anti-inflammatory components include allantoin, calamine, tranexamic acid, glycyrrhizic acid or its derivatives or salts thereof (e.g., dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, etc.), glycyrrhetinic acid or its derivatives or salts thereof (e.g., glycyrrhetinic acid, stearyl glycyrrhetinate, etc.), zinc oxide, aminocaproic acid, azulene and its derivatives (e.g., guaiazulene, azulene, etc.), tocopherol acetate, pyridoxine hydrochloride, menthol, camphor, turpentine oil, indomethacin, salicylic acid or its derivatives, steroids or their derivatives or salts thereof (e.g., hydrocortisone, prednisolone), ufenamate, bufexamac, ibuprofen piconol, glycol salicylate, and components derived from plants (e.g., confetti, coptis japonica, houttuynia cordata).

[0066] Examples of antibacterial components include chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, ethanol, benzethonium chloride, cresol, gluconic acid and its derivatives, povidone-iodine, potassium iodide, iodine, isopropylmethylphenol, triclocarban, triclosan, photosensitizer 101, photosensitizer 201, parabens, phenoxyethanol, alkyldiaminoglycine hydrochloride, cetylpyridinium chloride, piroctoolamine, miconazole or its salts, chlorobutanol, ethylhexylglycerin, iodidepropynyl butylcarbamate, caprylhydroxamic acid, phenethyl alcohol, methylisothiazolinone, sorbic acid, β-glycyrrhetinic acid, and components derived from plants (e.g., Sophora flavescens, rosemary, mulberry, eucalyptus, etc.).

[0067] Examples of cooling agents include menthol and its derivatives, terpenes such as camphor, bornol, geraniol, cineol, anetol, limonene, and eugenol (these may be d-isomers, l-isomers, or dl-isomers); and essential oils such as eucalyptus oil, bergamot oil, peppermint oil, coolmint oil, spearmint oil, fennel oil, peppermint oil, cinnamon oil, rose oil, and turpentine oil.

[0068] Examples of organic acids include gluconic acid, aspartic acid, aminoethylsulfonic acid, citric acid, glutamic acid, succinic acid, oxalic acid, fumaric acid, malonic acid, maleic acid, propionic acid, malic acid, salicylic acid, glycolic acid, phytic acid, tartaric acid, acetic acid, lactic acid, pantothenic acid, glycyrrhetinic acid, alginic acid, ascorbic acid, benzoic acid, adipic acid, glutamic acid, azelaic acid, and salts thereof.

[0069] Examples of anti-glycation ingredients include plant extracts such as Budreja axillaris leaf extract, plum fruit extract, and edelweiss extract, evening primrose oil, amla fruit, fruit juice or extracts thereof, L-arginine, L-lysine, hydrolyzed casein, hydrolyzed tannins, and carnosine.

[0070] Examples of cell-activating components include amino acids such as γ-aminobutyric acid and ε-aminocaproic acid; vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride, and pyrroloquinoline quinones of pantothenate; α-hydroxy acids such as gluconic acid, phytic acid, glycolic acid, and lactic acid; tannins, flavonoids, saponins, allantoin, photosensitizer 301, and components derived from plants (e.g., soybean sprouts, bilberry leaves, etc.).

[0071] Examples of astringent components include metal salts such as alum, chlorohydroxyaluminum, aluminum chloride, allantoin aluminum salt, zinc paraphenolsulfonate, basic aluminum zinc lactate, zinc sulfate, and aluminum potassium sulfate; and organic acids such as tannic acid, citric acid, lactic acid, and succinic acid.

[0072] Examples of antioxidants include butylhydroxyanisol, dibutylhydroxytoluene, sodium bisulfite, sodium pyrosulfite, erythorbic acid and its salts, ascorbic acid and its salts, flavonoids, glutathione, glutathione peroxidase, glutathione-S-transferase, catalase, superoxide dismutase, thioredoxin, taurine, thiotaurine, hypotaurine, and plant extracts (such as honeysuckle flower extract).

[0073] Examples of anti-aging ingredients include hydrolyzed soy protein, retinoids (retinol, retinoic acid, retinal, etc.), pangamic acid, ursolic acid, turmeric extract, sphingosine derivatives, silicon, silicic acid, N-methyl-L-serine, mevalonolactone, and peptides (caprooyl tetrapeptide-3, oligopeptide-24, etc.).

[0074] Moisturizing ingredients include, for example, amino acids and their derivatives such as alanine, serine, aspartic acid, glycine, proline, hydroxyproline, glucosamine, theanine, and arginine; polyhydric alcohols such as glycerin, dipropylene glycol, and 1,3-butanediol; sugar alcohols such as sorbitol, xylitol, erythritol, and maltose-sucrose condensate (gluco-oligosaccharide); glycosyltrehalose, trehalose; ceramide, glucosylceramide, Examples include cholesterol, phytosterol, cholesterol derivatives, phytosterol derivatives; phospholipids such as lecithin and hydrogenated lecithin; NMF-derived components such as lactic acid, sodium lactate, sodium pyrrolidone carboxylate, and urea; collagen, elastin, keratin, chitin, chitosan, and their hydrolysates; hydroxyethyl urea; and components derived from plants (for example, chamomile, witch hazel, tea, perilla, grapefruit, Gynostemma pentaphyllum, etc.). In particular, combinations with one or more selected from glycine, arginine, glycerin, dipropylene glycol, 1,3-butanediol, glycosyltrehalose, ceramide, glucosylceramide, cholesterol, cholesterol derivatives, phytosterol derivatives, hydrogenated lecithin, lactic acid, sodium lactate, sodium pyrrolidone carboxylate, urea, collagen, elastin, keratin, and hydroxyethyl urea are preferred.

[0075] Examples of polyhydric alcohols include diols with 2 to 4 or 11 or more carbon atoms, and polyhydric alcohols having 3 or more hydroxyl groups. Examples include glycerin, diglycerin, triglycerin, propylene glycol, dipropylene glycol, 1,3-butanediol, ethylene glycol, diethylene glycol, isoprene glycol, and 1,3-butylene glycol.

[0076] Examples of keratin-softening ingredients include lanolin, urea, phytic acid, lactic acid, lactate, glycolic acid, salicylic acid, malic acid, citric acid, fruit acid, phytic acid, urea, sulfur, and others.

[0077] Examples of vitamins include retinol derivatives such as retinolic acid and retinoyl linoleate, vitamin A derivatives such as retinal, retinoic acid, methyl retinoate, ethyl retinoate, retinoic acid, d-δ-tocopheryl retinoate, α-tocopheryl retinoate, and β-tocopheryl retinoate; and provitamin A derivatives such as β-carotene, α-carotene, γ-carotene, δ-carotene, lycopene, zeaxanthin, cryptoxanthin, and echinenone. Vitamin E derivatives such as linoleic acid tocopherol, (linoleic acid / oleic acid) tocopherol, (ascorbyl / tocopheryl) potassium phosphate; Vitamin B2 derivatives such as riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, riboflavin 5'-phosphate sodium, riboflavin tetranicotinate; and methyl nicotinate, nicotinic acid, benzyl nicotinate, etc. (A) Other nicotinic acids; Vitamin C compounds such as ascorbyl stearate, disodium isostearyl ascorbyl phosphate, L-ascorbyl dipalmitate, ascorbyl tetraisopalmitate (tetra-2-hexyldecanoate ascorbyl), trisodium ascorbyl palmitate phosphate, ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbate phosphate, magnesium ascorbate phosphate, ascorbic acid glucoside, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, glyceryl ascorbate, bisglyceryl ascorbate, alkylglyceryl ascorbate; Vitamin D compounds such as methyl hesperidin, ergocalciferol, cholecalciferol; Vitamin K compounds such as phylloquinone, farnoquinone; Thiamine and their salts (e.g., diben Vitamin B1s such as zoylthiamine hydrochloride, thiamine hydrochloride, thiamine diphosphate; Vitamin B6s such as pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, pyridoxal 5'-phosphate, pyridoxamine hydrochloride; Vitamin B12s such as cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin; Folic acid derivatives such as folic acid and pteroylglutamic acid; Pantothenic acid, calcium pantothenate, pantothenylal Examples include pantothenic acids such as chol (panthenol), D-pantetheine, D-pantethine, coenzyme A, pantothenyl ethyl ether, and calcium pantetheine sulfonate; biotins such as biotin and biocitin; and other vitamin-like factors such as carnitine, ferulic acid, alpha-lipoic acid, orotic acid, gamma-oryzanol, pyrroloquinoline quinone, hesperidin and glucosyl herperidin, ubiquinone, and their salts.

[0078] Examples of blood circulation-promoting ingredients include those derived from plants (e.g., ginseng, angelica tree, arnica, ginkgo, fennel, laurel, watercress, chamomile, Roman chamomile, carrot, gentian, burdock, rice, hawthorn, shiitake mushroom, hawthorn, juniper, cinnamon, gentian, thyme, clove, dried tangerine peel, angelica, peach kernel, spruce, carrot, garlic, butcher's broom, grape, peony, horse chestnut, lemon balm, yuzu, coix seed, rosemary, rosehip, dried tangerine peel, angelica, spruce, peach, apricot, walnut, corn); dl-α-tocopherol acetate, tocopherol nicotinate, glucosyl hesperidin, and hesperidin.

[0079] Examples of sebum-absorbing components include talc, mica, hydroxyapatite, zinc oxide, and aluminum silicate. Among these, mica, hydroxyapatite, and zinc oxide are preferred, and mica is particularly preferred.

[0080] Examples of peptides or their derivatives include keratin-degrading peptides, hydrolyzed keratin, collagen, fish-derived collagen, atelocollagen, succinylated atelocollagen, gelatin, elastin, elastin-degrading peptides, collagen-degrading peptides, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin-degrading peptides, conchiolin-degrading peptides, hydrolyzed conchiolin, silk protein-degrading peptides, hydrolyzed silk, sodium lauroyl hydrolyzed silk, soy protein-degrading peptides, hydrolyzed soy protein, wheat protein, wheat protein-degrading peptides, hydrolyzed wheat protein, casein-degrading peptides, and acylated peptides (palmitoyl oligopeptides, palmitoyl pentapeptides, palmitoyl tetrapeptides, etc.).

[0081] Examples of amino acids or their derivatives include betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, β-alanine, threonine, glutamic acid, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine, leucine, isoleucine, valine, histidine, threonine, tyrosine, taurine, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine, creatine, epsilonaminocaproic acid, tryptophan, ornithine, sodium N-stearoyl-L-glutamate, dilauroyl glutamate lysine and its salts, lauroyl glutamate di(phytosteryl / octyldodecyl), lauroyl glutamate di(octyldodecyl / phytosteryl / behenyl), and the like. These amino acids or their derivatives may also be solvates such as hydrates, and may be d-isomers, l-isomers, or dl-isomers. Among these, one or more selected from l-isomer amino acids or their derivatives are preferred.

[0082] Furthermore, in addition to the above-mentioned components, the external composition of the present invention may appropriately contain components commonly used in the fields of pharmaceuticals, quasi-drugs, or cosmetics, depending on its use or dosage form. There are no particular limitations on the components that can be included, but for example, additives such as bases or carriers, surfactants, thickeners, antioxidants, preservatives, pH adjusters, chelating agents, stabilizers, irritation reducers, colorants, dispersants, and fragrances can be included. These components can be included individually or in any combination of two or more. The content of these components can be appropriately determined within a range that does not impair the effects of the present invention, based on conventionally known ranges. Furthermore, components falling under any of the following multiple categories may be added as components with any of the functions among them.

[0083] The base or carrier may be an aqueous base such as water; hydrocarbons such as petrolatum, paraffin, microcrystalline wax, polybutene, polyethylene powder, gelled hydrocarbons (such as Plastibase), ozokerite; phenyl-modified silicon such as highly polymerized methylpolysiloxane, cyclic silicon, methylhydrogenpolysiloxane, methyl trimethicone, dimethiconol, dimethiconol crosspolymer, caprylyl methicone, etc., alkyl-modified silicon, cross-linked alkyl-modified silicon, amino-modified silicon, polyethylene-modified silicon, polyg Silicone oils such as ricerin-modified silicone, cross-linked polyethylene-modified silicone, cross-linked alkyl polyethylene-modified silicone, silicone-alkyl chain-comodified polyethylene-modified silicone, silicone-alkyl chain-comodified polyglycerin-modified silicone, polyethylene-modified branched silicone, polyglycerin-modified branched silicone, acrylic silicone, phenyl-modified silicone, and silicone resin; higher alcohols such as cetanol, cetostearyl alcohol, stearyl alcohol, behenyl alcohol, phytosterol, and cholesterol; Higher fatty acids such as uric acid, myristic acid, palmitic acid, stearic acid, and behenic acid; cellulose derivatives such as ethyl cellulose, hydroxypropyl cellulose, and hydroxypropyl methylcellulose; polyvinylpyrrolidone; polyvinyl butyrate; polyethylene glycol; dioxane; butylene glycol adipate polyester; cetyl lactate, dextrin palmitate, inulin stearate, tri-2-ethylhexyl trimellitate, tridecyl trimellitate, tri(caprylic / capric / myristic / stearic acid) Esters such as glyceryl, phytosteryl / octyldodecyl lauroyl glutamate, octyldodecyl / phytosteryl / behenyl lauroyl glutamate, phytosteryl / isostearyl / cetyl / stearyl / behenyl dimer-dilinoleate, dimer-dilinoleyl dimer-dilinoleate, dipentaerythrityl tripolyhydroxystearate, and glyceryl tri(behenate / isostearate / eicosanedioate); waxes such as miura wax, candelilla wax, rice bran wax, cotton wax, carnauba wax, and lanolin; oils and fats;Examples include polysaccharides such as dextrin and maltodextrin; vinyl polymers such as carboxyvinyl polymers and alkyl-modified carboxyvinyl polymers; lower alcohols such as ethanol and isopropanol; sugar alcohols such as sorbitol, xylitol, erythritol, and mannitol; and water. These components may be used individually as a base or carrier, or in combination of two or more. The amounts used can be appropriately selected from a range known to those skilled in the art.

[0084] When the topical composition of the present invention contains water, the amount of water it contains varies depending on the form of the topical composition and is not particularly limited. For example, the amount of water relative to the total amount of the topical composition of the present invention is preferably 10 to 99% by mass, more preferably 50 to 95% by mass, and even more preferably 60 to 90% by mass.

[0085] When the topical composition of the present invention contains an oil other than (D) liquid oil as a base, the amount of the oil other than (D) liquid oil varies depending on the form of the topical composition and is not particularly limited. For example, the amount of the oil other than (D) liquid oil relative to the total amount of the topical composition of the present invention is preferably 0.0001 to 5% by mass, more preferably 0.001 to 1% by mass, and even more preferably 0.005 to 0.5% by mass.

[0086] Examples of surfactants include sorbitan fatty acid esters such as sorbitan monoisostearate, sorbitan monostearate, sorbitan diglycerol sorbitan tetra-2-ethylhexylate, sorbitan monooleate, sorbitan monoisostearate, and sorbitan monolaurate; polyoxyethylene (20) sorbitan monolauryl acid, polyoxyethylene (80) sorbitan monolauryl acid, polyoxyethylene (20) sorbitan monostearate, and polyoleate monooleate. Polyoxyethylene sorbitan fatty acid esters such as oxyethylene(20) sorbitan and polyoxyethylene(20) sorbitan isostearate; glycerin fatty acid esters such as glycerin monooleate, glycerin monostearate, and glycerin monomyristate; glycerin alkyl ethers such as monoisostearylglyceryl ether and monomyristylglyceryl ether; diglyceryl monostearate, decaglyceryl decastearate, decaglyceryl decaiso Polyglycerin fatty acid esters such as stearete and diglyceryl diisostearate; propylene glycosate fatty acid esters such as propylene glycosate monostearate; hydrogenated castor oil derivatives such as polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 50, polyoxyethylene hydrogenated castor oil 60, and polyoxyethylene hydrogenated castor oil 80; polyoxyethylene glycerin fatty acid esters such as polyoxyethylene monococonut oil fatty acid glyceryl; polyoxyethylene Polyoxyethylene sterols and hydrogenated sterols such as len(20)phytosterol, polyoxyethylene(30)phytosterol, polyoxyethylene(25)phytostanol, and polyoxyethylene(30)cholestanol; sucrose fatty acid esters; polyoxyalkylene alkyl (or alkenyl) ether sulfates, ether carboxylates, alkyl phosphate esters, N-acyl amino acid salts, acylated taurates; amines such as stearylamine and oleylamine;Examples include silicate-based surfactants such as polyoxyethylene-methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, and PEG-9 polydimethylsiloxyethyl dimethicone, as well as naturally derived surfactants such as lecithin, hydrogenated lecithin, saponins, sodium surfactant, cholesterol, and bile acids.

[0087] Examples of thickening agents include vinyl-based thickening agents such as polyacrylamide, polyvinyl alcohol, polyvinylpyrrolidone, polyvinyl methyl ether, and carboxyvinyl polymer, as well as methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, carboxymethylcellulose, and carboxyethylcellulose. Examples include cellulose-based thickeners such as guar gum, sclerotium gum, tamarind gum, xanthan gum, dextran, pectin, pullulan, gelatin, locust bean gum, carrageenan, agar, alkyl acrylate methacrylate copolymer, sodium polyacrylate, bentonite, dextrin fatty acid ester, dimethyldistearylammonium hectorite, sodium alginate, propylene glycol alginate ester, polyethylene glycol, macrogol, (hydroxyethyl acrylate / sodium acryloyldimethyltaurate) copolymer, (ammonium acryloyldimethyltaurate / vinylpyrrolidone) copolymer, etc.

[0088] Examples of antioxidants include dibutylhydroxytoluene, butylhydroxyanisol, sorbic acid, sodium sulfite, ascorbic acid, ascorbic acid derivatives, tocopherol, tocopherol derivatives, erythorbic acid, sodium erythorbate, L-cysteine ​​hydrochloride, ubiquinones such as coenzyme Q10, lignans such as sesamin, curcumin, capsaicin, gingerol, resveratrol, anthocyanins, cyanidin, bilberry extract, and their analogs or derivatives.

[0089] Examples of preservatives or antimicrobial agents include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl parahydroxybenzoate, isopropyl parahydroxybenzoate, butyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, benzyl parahydroxybenzoate, methyl parahydroxybenzoate, phenoxyethanol, benzyl alcohol, chlorobutanol, sorbic acid and its salts, chlorhexidine gluconate, methylisothiazolinone, iodide propynyl butylcarbamate, caprylhydroxamic acid, phenethyl alcohol, ethylhexylglycerin, glyceryl caprate, isopropylmethylphenol, and the like.

[0090] Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide, sodium hydroxide, etc.), and organic bases (triethanolamine, diisopropanolamine, triisopropanolamine, etc.).

[0091] Examples of chelating agents include ethylenediaminetetraacetic acid (EDTA), ethylenediaminetetraacetic acid salts (sodium salt (sodium edetate: Japanese Pharmacopoeia, EDTA-2Na, etc.), potassium salt, etc.), phytic acid, gluconic acid, polyphosphate, metaphosphate, etc. Among these, sodium edetate is preferred.

[0092] Examples of stabilizers include sodium polyacrylate, dibutylhydroxytoluene, and butylhydroxyanisol.

[0093] Examples of irritation-reducing agents include licorice extract, gum arabic, and polyvinylpyrrolidone.

[0094] [pH] The topical composition of the present invention may normally have a pH of 4 to 9, but from the viewpoint of low irritation to the skin and mucous membranes and good skin feel, it is preferably pH 4.5 to 8.5, more preferably pH 5 to 8, and even more preferably pH 6 to 8.

[0095] [Method for Manufacturing the Topical Composition] The method for manufacturing the topical composition of the present invention is not particularly limited. In addition to the above components (A) to (D), other components may be appropriately selected and blended, and the composition may be manufactured by conventional methods, with emulsification if necessary.

[0096] [Uses] When used as an external composition for quasi-drugs or cosmetics, specific uses include, for example, basic cosmetics such as lotions, emulsions, gels, creams, serums, sunscreens, packs, masks, hand creams, and body lotions; cleansing cosmetics such as facial cleansers, hand soaps, makeup removers, body shampoos, shampoos, rinses, and treatments; face makeup cosmetics such as foundations and makeup bases; and hair cosmetics such as hair gels, hair mousses, hair mists, hair lotions, and styling products. Among these, external compositions for skin use are particularly preferred. In other words, the external composition of the present invention can be an external composition for pharmaceuticals, quasi-drugs, or cosmetics. The formulation form of the external composition is the same as that of the external composition of the present invention. Furthermore, the usable bases or carriers, additives, and active ingredients, as well as preferred ones thereof, are the same as those of the external composition of the present invention. Among these, formulations selected from lotions, emulsions, gels, serums, sunscreens, packs, masks, hand creams, body lotions, hair gels, hair mists, and hair lotions are more preferred. Furthermore, application to lotions, emulsions, gels, serums, sunscreens, and masks is even more preferred because it particularly affects the appearance of the formulation due to its transparency, which is one of the effects of the present invention.

[0097] [Container] The external composition of the present invention can be contained in a container of a shape and material appropriately selected according to the purpose and use. Examples of specific containers include spray type, bottle type, tube type, jar type, dropper type, dispenser type, stick type, pouch bag, and chia pack.

[0098] Examples of container materials include polyethylene terephthalate, polypropylene, polyethylene (HDPE, LDPE, LLDPE, etc.), ABS resin, ethylene vinyl alcohol resin, polystyrene, glass, and metals (aluminum, etc.). These materials can be used as container materials by applying various coating treatments, mixing or combining them, or laminating them, taking into consideration their strength, flexibility, weather resistance, or component stability. Examples of coating materials include epoxy resin and polyamide-imide. Among these, polypropylene, polyethylene (HDPE, LDPE, LLDPE, etc.), ethylene vinyl alcohol resin, and metals (aluminum, etc.) are preferred.

[0099] [Method of Use, etc.] The topical composition of the present invention can be suitably used for moisturizing, anti-inflammatory, chilblains, treatment and prevention of hypertrophic scars and keloids, progressive palmar and plantar keratoderma, cortical deficiency, and swelling, hematoma, tenosynovitis, muscle pain, and arthritis after trauma (bruises, sprains, contusions), taking advantage of the physiological activity of heparinoid. Furthermore, it can also be expected to improve barrier function, making it a useful multi-functional formulation. The topical composition of the present invention can be used once to several times a day, depending on the application, in known or commonly used dosages and administrations. [Examples]

[0100] Next, the present invention will be specifically described with reference to examples, but the present invention is not limited to the following examples. Also, unless otherwise specified, the units of the numerical values ​​in each table are weight (%).

[0101] [Examples 1-3, Comparative Examples 1-6] The compositions of the formulations shown in Table 1 below were prepared by conventional methods. [Table 1] TIFF0007893582000001.tif2769

[0102] [Test Example 1-1: Immediately After Preparation (Transparency Evaluation)] The transparency of the compositions of Example 1 and Comparative Examples 1 and 2 shown in Table 1 above was evaluated immediately after preparation under the following measurement conditions. The results are shown in Table 2 below. [Transparency Evaluation] The transparency of the formulations was evaluated by dispensing 200 μL of each composition into a 96-well plate (SBS standard) and measuring the absorbance at 630 nm using a microplate Retriever (SH-9000, Corona Electric Co., Ltd.) (measurement method: absorbance, measurement direction: ↑↑), according to the evaluation criteria below. As a control, the absorbance of purified water was measured using the same method and a result of "-0.004" was obtained. [Transparency Evaluation Criteria] [Judgment]: [630 nm Absorbance] Transparent: Less than 0.01 Slightly translucent: 0.01 or more and less than 0.1 Translucent: 0.1 or more and less than 0.3 Opaque: 0.3 or more

[0103] [Test Example 1-2: Immediately After Manufacturing (Visual Evaluation of Transparency)] The compositions of Example 1 and Comparative Examples 1 and 2 shown in Table 1 above were evaluated for transparency immediately after preparation under the following measurement conditions. The results are shown in Table 2 below. [Visual Evaluation of Transparency] For visual evaluation of the transparency of the formulations, each composition was filled into a 30 mL glass screw-top bottle to a height of 3 cm, and the visibility and clarity of the characters in font 14 below the glass bottle could be evaluated according to the following evaluation criteria. [Visual Transparency Evaluation Criteria] [Judgment]: [Judgment Criteria] 5: The characters are very clearly visible, and the clarity is very high. 4: The characters are clearly visible, and the clarity is high. 3: The characters are visible, but the clarity is somewhat poor. 2: The characters are barely visible, but the clarity is poor. 1: The characters are illegible, and the product is opaque. [Table 2] TIFF0007893582000002.tif1470

[0104] As shown in the results in Table 2, in Test 1-1, Example 1 showed absorbance equivalent to that of the purified water described as a reference example, and visual inspection of its appearance also showed it to be colorless and transparent, equivalent to the reference example, with no difference observed in the visibility of the text. Comparative Examples 1 and 2 were formulated with a different component belonging to the same mucopolysaccharide class instead of component (A) of Example 1. Comparative Example 1 was in the opaque category in terms of absorbance values ​​in Test 1-1, and visual inspection of the text in Test 2-2 did not allow for recognition of the text. Comparative Example 2 was in the semi-transparent category in terms of absorbance values ​​in Test 1-1, and visual inspection of the text in Test 2-2 showed that although the text was visible, its clarity was considerably inferior to that of Example 1.

[0105] [Test Examples 1-3: Appearance and Appearance Stability (Transparency)] 50g of each composition of the formulations shown in Table 1 (Examples 1-3, Comparative Examples 1-6) was filled into 50mL glass screw-cap bottles, and a thermal stability test (3 days) at 60°C and a photostability test (260,000 LUX irradiation) were performed. (Test conditions) Thermal stability test conditions: Stored in a 60°C constant temperature chamber for 3 days. Photostability test conditions: At 25°C, light from a D65 fluorescent lamp, a standard light source defined by the International Commission on Illumination (CIE), was irradiated at 3800 LUX / h for approximately 69 hours (total 260,000 LUX·hr). After the completion of each stability test, the samples were kept at a constant temperature of 25°C, and the transparency and appearance (transparency) stability under each stability test condition were evaluated according to the following measurement conditions. A comprehensive judgment regarding appearance stability was also made based on the results of the thermal stability test and the photostability test. These results are shown in Table 3. Furthermore, for each composition of the formulations shown in Table 1 above (Examples 2-3, Comparative Examples 3-6), the transparency immediately after preparation was also evaluated according to Test 1-2 described above, and the results are shown in Table 3. [Evaluation of Transparency] The transmittance of the formulations was evaluated by dividing each composition into a 96-well plate (SBS standard) and measuring the absorption spectrum using a microplate retriever (SH-9000, Corona Electric Co., Ltd.) (measurement method: absorbance, measurement direction: →→), according to the evaluation criteria below. (Evaluation criteria for transparency immediately after manufacturing (absorption spectrum measurement)) [Judgment]: [630nm absorbance] Transparent: -0.5 or higher Slightly translucent: -2 or higher and less than -0.5 Translucent: -5 or higher and less than -2 Opaque: Less than -5

[0106] (Evaluation Criteria for Appearance Stability (Transparency) (Absorption Spectrum Measurement)) Appearance Stability (Transparency) (Difference in 630nm Absorbance) = Value after Stability Test - Initial Value [Difference in 630nm Absorbance]: [Judgment] 5 or more: Appearance stability is reduced 1 or more, less than 5: Appearance stability is slightly reduced -1 or more, less than 1: Appearance stability is good -3 or more, less than -1: Appearance stability is slightly reduced -6 or more, less than -3: Appearance stability is reduced -6 less: Appearance stability is significantly reduced (Overall Judgment of Appearance Stability (Transparency)) [Appearance Stability (Transparency): Judgment] ◎: Both thermal and photostable are stable ○: Either thermal or photostable is slightly reduced △: Either thermal or photostable is reduced or both are slightly reduced X: Either thermal or photostable is significantly reduced or both are reduced

[0107] (Stability of appearance (maintenance of transparency)) Regarding the stability of appearance of this invention, the lower the absorbance value at 630 nm in the absorption spectrum measurement, the lower the transmittance, meaning that the transparency is lower. Therefore, the larger the negative difference between the absorbance after the stability test and the initial value, the lower the transparency (worsening of turbidity), meaning that the stability of appearance is poor. On the other hand, the larger the difference in absorbance, the higher the transmittance, meaning that the appearance changes due to increased transparency, and therefore the stability of appearance is poor. Thus, the closer the difference in absorbance before and after the test is to 0, the more stable the appearance (maintaining transparency) is.

[0108] As shown in Table 3, in the examples where gellan gum, another polysaccharide, was used instead of component (A) in Examples 1-3 (Comparative Examples 1, 3, and 5), the absorbance after testing showed an increasing trend in both thermal and light stability, indicating poor appearance stability (transparency). In the examples where agar was used (Comparative Examples 2, 4, and 6), the absorbance decreased in both thermal and light stability, meaning transparency decreased, indicating a significant deterioration in appearance stability (transparency). The Examples were stable in both the light and thermal stability tests, and their appearance stability (transparency) was maintained.

[0109] [Test Example 1-4: Stability (Coloring)] The same test samples as in Test Example 1-3 were used to evaluate the stability (coloring). [Evaluation of Stability (Coloring)] The coloring of the formulation was evaluated by separating each composition into a 96-well plate (SBS standard), measuring the absorption spectrum using a microplate recorder (SH-9000, manufactured by Corona Electric Co., Ltd.) (measurement method: absorbance, measurement direction: →→), and using the absorbance at 450 nm, according to the evaluation criteria below. (Color Stability Evaluation Criteria) Stability (Color) (Difference in 450nm absorbance) = Value after stability test - Initial value [Difference in 450nm absorbance]: [Judgment] 1 or more: Stability (color) is slightly decreased -1 or more Less than 1: Stability (color) is good -3 or more, less than -1: Stability (color) is slightly decreased -6 or more, less than -3: Stability (color) is decreased Less than -6: Stability (color) is considerably decreased (Overall judgment of appearance stability (transparency)) [Appearance stability (transparency): Judgment] ◎: Both thermal and light stability are stable ○: Either thermal or light stability is slightly decreased △: Either thermal or light stability is decreased or both are slightly decreased X: Either thermal or light stability is considerably decreased or both are decreased

[0110] (Stability (Coloring)) Regarding the stability (coloring) of the present invention, the lower the absorbance value at 450 nm in the absorption spectrum measurement, the more yellow the color of the formulation is. Therefore, the larger the negative value obtained by subtracting the initial value from the absorbance after the stability test, the worse the yellowing has become, and the poorer the stability (coloring). On the other hand, the larger the difference in absorbance as described above, the lighter the color of the formulation becomes, and the change in appearance has occurred, which means that the stability (coloring) is poor. Therefore, the closer the difference in absorbance before and after the test is to 0, the better the stability (coloring) is.

[0111] As shown in Table 3, in the examples where gellan gum, one of the polysaccharides, was used instead of component (A) in Examples 1-3, and in the example where 1,2-pentanediol was used instead of component (B) in Comparative Example 5, the absorbance after the test increased, indicating poor stability (transparency) of appearance. Similarly, in the examples where agar was used (Comparative Examples 2, 4, and 6), the formulations yellowed significantly in both thermal and light stability tests, indicating a significant decrease in stability (coloring). In contrast, all of the examples showed no yellowing in either the light test or the thermal stability test, demonstrating excellent stability (coloring).

[0112] [Test Example 1-5: Stability (pH)] The stability (pH) was evaluated using the same thermal stability test sample as in Test Example 1-3. (pH Stability Evaluation Criteria) Stability (pH) = Measured value after stability test - Initial value [Stability (pH)] : [Judgment] 1 or higher: Stability (coloring) slightly decreased ±0.2 or less: ◎ ~ ±0.3 or less: ○ ~ ±0.4 or less: △ ±0.5 [ : X [Table 3] TIFF0007893582000003.tif5066

[0113] As shown in Table 3, the examples in which gellan gum, another polysaccharide, was used instead of component (A) in Examples 1-3, and the examples in which agar was used (Comparative Examples 2, 4, and 6), showed a tendency for the pH to decrease. In particular, the examples in which agar was used (Comparative Examples 2 and 4) showed a greater tendency for stability (pH) to decrease. On the other hand, none of the examples showed a significant change in pH, indicating good stability (coloring).

[0114] [Test Example 1-6: User Experience (Stickiness, Slipperiness, Penetration)] For each composition of the formulation shown in Table 1 above, the user experience (stickiness, slipperiness, penetration) was evaluated by three dedicated panelists according to the evaluation criteria below. When an appropriate amount (approximately 0.05g) of each test formulation was applied to a 2cm x 2cm area on the inside of the arm of six expert panelists, the user experience was scored on a 3-point scale according to the following items and criteria, and the values ​​were averaged. The results are shown in Table 4. (Stickiness) 3: Not sticky. 2: Slightly sticky. 1: Sticky. (Slippery) 3: Not slimy. 2: Slightly slimy. 1: Slimy. [Table 4] TIFF0007893582000004.tif1370

[0115] As shown in Table 4, compared to Comparative Example 1, which contained gellan gum instead of component (A) of Example 1, and Comparative Example 2, which contained agar, Example 1, which contained heparinoid (A), had a better feel in terms of stickiness and sliminess when combined with component (B).

[0116] [Test Example 2-1] The compositions of the formulations shown in Table 5 below were prepared by conventional methods. The prepared compositions were evaluated for transparency, stability (appearance (transparency), color, pH), and usability immediately after manufacturing, according to the test conditions of Test Examples 1-1 to 1-6 described above. The results are shown in Table 4. [Table 5] TIFF0007893582000005.tif5630

[0117] As shown in Table 5, for Example 4, favorable results were obtained in all evaluation items.

[0118] [Formulation Examples] Based on the formulations in Tables 6 to 31 below, the topical skin compositions of the present invention (Formulation Examples 1 to 26) were prepared.

[0119] [Table 6] (Formulation Example 1: Lotion 1) TIFF0007893582000006.tif6439

[0120] [Table 7] (Formulation Example 2: Lotion 2) TIFF0007893582000007.tif4940

[0121] [Table 8] (Example of formulation 3: Lotion 3) TIFF0007893582000008.tif6843

[0122] [Table 9] (Formulation Example 4: Lotion 4) TIFF0007893582000009.tif5840

[0123] [Table 10] (Formulation Example 5: Impregnated Sheet Mask) TIFF0007893582000010.tif6641

[0124] [Table 11] (Formulation Example 6: Mist Spray) TIFF0007893582000011.tif5840

[0125] [Table 12] (Formulation Example 7: pH 6 O / W Lotion) TIFF0007893582000012.tif7540

[0126] [Table 13] (Formulation Example 8: pH 6.5 O / W Lotion) TIFF0007893582000013.tif7340

[0127] [Table 14] (Formulation Example 9: pH 6.3 O / W Hand Lotion) TIFF0007893582000014.tif6540

[0128] [Table 15] (Formulation Example 10: pH 6.3, All-in-One Gel) TIFF0007893582000015.tif6842

[0129] [Table 16] (Formulation Example 11: pH 6.5 Sunscreen Gel Lotion) TIFF0007893582000016.tif7150

[0130] [Table 17] (Formulation Example 12: Beauty Serum) TIFF0007893582000017.tif6843

[0131] In all of the formulation examples, the compositions were excellent, with no stickiness and a superior feel during use.

Claims

1. (A) Heparin-like substances, (B) One or more selected from the group consisting of 1,3-propanediol, 1,2-pentanediol, and 1,2-hexanediol, and One or more selected from the group consisting of diethoxyethyl succinate, bisethoxydiglycol cyclohexanedicarboxylic acid, polyoxyalkylene glyceryl ether, polyoxypropylene methyl glucoside, polyoxypropylene alkyl ether, polyoxyalkylene sorbit, polyoxyalkylene erythritol ether, polyoxyalkylene pentaerythritol ether, polyoxyalkylene diglyceryl ether, polyoxyalkylene trimethylolpropane, polyoxypropylene glyco, polyoxyethylene polyoxypropylene glyco, polyoxyalkylene xylitol, polyoxyalkylene dipentaerythritol, polyoxyalkylene inositol, polyoxyalkylene sucrose ether, polyoxyalkylene trehalose ether, and polyoxyalkylene maltoitol ether. An external composition comprising the above, wherein the content of component (A) is 0.01 to 5% by mass, and the content of component (B) is 0.01 to 30% by mass.

2. The topical composition according to claim 1, further comprising one or more components selected from the group consisting of (C) glycyrrhizinate, water-soluble ascorbic acid derivatives, and tranexamic acid.

3. The topical composition according to claim 2, wherein component (C) contains one or more selected from the group consisting of dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, sodium ascorbate phosphate, magnesium ascorbate phosphate, 2-O-ethyl ascorbic acid, 3-O-ethyl ascorbic acid, ascorbic acid glucoside, and tranexamic acid.

4. The external composition according to any one of claims 1 to 3, further comprising component (D) liquid oil.

5. The topical composition according to any one of claims 1 to 4, characterized in that the topical composition is liquid.

6. The topical composition according to any one of claims 1 to 5, characterized in that the viscosity of the topical composition is 10 to 10,000 mPa·s.

7. The topical composition according to any one of claims 1 to 6, characterized in that the appearance of the topical composition is transparent to semi-transparent.

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